Tozasertib, Free Base (N-[4-[[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanyl]phenyl]cyclopropanecarboxamide, VX-680, MK-0457, VX6)

Tozasertib is a potent inhibitor of all aurora kinases, including the A, B and C isotypes (Ki=0.6nM, 18nM and 4.6nM, respectively). It also inhibits ABL kinase (Ki=30nM), an imatinib-resistant ABL mutant (T315I) kinase (Ki=42nM), and Flt-3 (Ki=30nM). Tozasertib binds to an inactive aurora conformation.\n\nSolubility:\nSoluble in DMSO at 100mg/ml; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-30uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

T8078

Size

10mg

Form

Supplied as a white to off-white powder.

Purity

~99%

References

1. Cheetham, G.M., et al. \"Structural basis for potent inhibition of the aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680.\" Cancer Lett. 251:323-329 (2007). 2. Carter, T.A., et al. \"Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.\" Proc. Natl. Acad. Sci. USA 102:11011-11016 (2005). 3. Harrington, E.A., et al. \"VX-680, a potent and selective small-molecule inhibitor of the aurora kinases, suppresses tumor growth in vivo.\" Nat. Med. 10:262-267 (2004). 4. Giles, F.J., et al. \"MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.\" Blood 109:500-502 (2007).